Pharmacological effect
An antibiotic of the macrolide group, it is a representative of the azalides. It suppresses RNA-dependent protein synthesis of sensitive microorganisms. Active against gram-positive bacteria: Staphylococcus aureus, Streptococcus spp. (including Streptococcus pneumoniae, Streptococcus pyogenes / group A /); gram-negative bacteria: Haemophilus influenzae, Haemophilus parainfluenzae, Haemophilus ducreyi, Moraxella catarrhalis, Escherichia coli, Bordetella pertussis, Bordetella parapertussis, Borrelia burgdorferi, Neisseria gonlorhoeae s, Campella, Bacteroides fragilis. Azithromycin is also active against Chlamydia trachomatis, Mycoplasma pneumoniae, Mycoplasma hominis, and Treponema pallidum. It is also active against Toxoplasma gondii.
Pharmacokinetics
It is rapidly absorbed from the gastrointestinal tract. Food intake reduces the absorption of azithromycin. Cmax in plasma is achieved in 2-3 hours. It is rapidly distributed in tissues and biological fluids. 35% of azithromycin is metabolized in the liver by demethylation. More than 59% is excreted in the bile unchanged, about 4.5% – in the urine unchanged.
Indications
Infections of the respiratory tract and ENT organs (tonsillitis, sinusitis, otitis media, pharyngitis, bronchitis, tracheitis, pneumonia), soft tissues (infectious myositis, bursitis, soft tissue wounds, etc.), the genitourinary system (cystitis, urethritis, cervicitis, gonococcal infection, etc.), stomach ulcer, duodenal ulcer, etc.
Contraindications
Hypersensitivity to antibiotics of the macrolide group. Severe liver and kidney dysfunctions. Pregnancy. Breastfeeding (suspended for the duration of treatment). It is used with caution in case of severe violations of the liver, kidneys, cardiac arrhythmias (ventricular arrhythmias and lengthening of the interval are possible).
Precautions
From the digestive system: nausea, vomiting, flatulence, diarrhea, abdominal pain, a transient increase in the activity of liver enzymes; rarely cholestatic jaundice. Allergic reactions: rarely – skin rash, angioedema, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis. Dermatological reactions: rarely – photosensitization. From the side of the central nervous system: dizziness, headache; rarely – drowsiness, weakness. From the hematopoietic system: rarely – leukopenia, neutropenia, thrombocytopenia. From the side of the cardiovascular system: rarely – chest pain. From the genitourinary system: vaginitis; rarely – candidiasis, nephritis, increased residual urea nitrogen.
Application during pregnancy and lactation
Azithromycin crosses the placental barrier. Use during pregnancy is possible only in cases where the intended benefit to the mother outweighs the potential risk to the fetus. If it is necessary to use azithromycin during lactation, the question of stopping breastfeeding should be resolved.
Method of administration and dosage
Inside, 1 time / day. The bioavailability of the tablets is independent of food intake. For infections of the upper and lower respiratory tract, skin and soft tissues (except for chronic migratory erythema): adults and children over 12 years old 500 mg 1 time / day for 3 days (course dose 1.5 g), children from 6 up to 12 years: at the rate of 10 mg / kg of body weight 1 time / day for 3 days (course dose of 30 mg / kg). In chronic migratory erythema, adults and children over 12 years old 1 time / day for 5 days: 1st day – 1.0 g (2 tablets of 500 mg), then from the 2nd to 5th day – 500 mg (course dose 3.0 d), children from 6 to 12 years old: on the 1st day – at a dose of 20 mg / kg of body weight and then from 2 to 5th day – daily at a dose of 10 mg / kg of body weight (course dose of 30 mg / kg ). For diseases of the stomach and duodenum associated with Helicobacter pylori: 1 g / day (2 tablets of 500 mg) for 3 days in combination with an antisecretory agent and other drugs. For sexually transmitted infections, uncomplicated urethritis / cervicitis – 1 g once, complicated, long-term urethritis / cervicitis caused by Chlamydia trachomatis – 1 g three times with an interval of 7 days (1-7-14). Heading dose 3 g.
Side effects
They are rare (in 1% of cases or less): From the gastrointestinal tract melena, cholestatic jaundice, bloating, nausea, vomiting, diarrhea, constipation, loss of appetite, gastritis. Allergic reactions, skin rashes. photosensitization, Quincke’s edema; on the part of the genitourinary system, vaginal candidiasis, nephritis; on the part of the cardiovascular system, palpitations, chest pain; on the part of the nervous system, dizziness, headache, vertigo, drowsiness, in children – headache (in the treatment of otitis media ), hyperkinesia, anxiety, neurosis, sleep disturbances. Other reversible moderate increases in the activity of liver enzymes, increased fatigue, itching, urticaria, conjunctivitis. In extremely rare cases, neutrophilia and eosinophilia.
The altered indicators return to the normal range 2-3 weeks after stopping treatment. You should inform your doctor about the occurrence of any side effect.
Overdose
Not recommended for use in patients with impaired liver function. Use with caution in case of impaired renal function. Azithromycin should be taken at least 1 hour before or 2 hours after meals or antacids.
Interaction with other drugs
With simultaneous use with ergot alkaloids, the risk of developing ergotism cannot be excluded. With the simultaneous use of azithromycin with warfarin, cases of increased effects of the latter are described. With the simultaneous use of digoxin or digitoxin with azithromycin, a significant increase in the concentration of cardiac glycosides in the blood plasma and the risk of developing glycosidic intoxication are possible. With simultaneous use with disopyramide, a case of ventricular fibrillation has been described. With simultaneous use with lovastatin, cases of the development of rhabdomyolysis have been described. With simultaneous use with rifabutin, the risk of developing neutropenia and leukopenia increases. With simultaneous use, the metabolism of cyclosporine is disrupted, which increases the risk of developing side and toxic reactions caused by cyclosporine.
Special instructions
Use with caution in case of impaired renal function.